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Chemical Compound Review:

AC1NSKN0 (2R)-5- (diaminomethylideneamino)-2- (2,2...

Synonyms: SureCN1593464, H 409-22

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High impact information on H 409-22

When guinea-pigs were pretreated with BIBO 3304 and H 409/22, the response to NPY was inhibited [1].
In the elevated plus-maze test, where novel neuropeptide Y Y(1) receptor antagonist (2R)-5-([amino(imino)methyl)amino)-2-[(2.2-diphenylacetyl)-amino]-N-[(1R)-1-(4-hydroxyphenyl)ethyl-pentanamide (H 409/22) had anxiogenic-like effect, CGP71683A was inactive [2].
In contrast, the NPY Y(2) receptor agonist N-acetyl[Leu(28)Leu(31)]NPY(24-36) (1.1 nmol kg(-1)), a dose of which potently evoked splenic NPY Y(2) receptor mediated (not affected by H 409/22) vasoconstriction, did not evoke any mesenteric vascular response [3].
During graded frequency renal sympathetic nerve stimulation (0 to 10 Hz), high-dose H 409/22 attenuated the decreases in renal blood flow only at 10 Hz (-36% +/- 5%, P <.05) in normal rats but did so at both 4 (-29% +/- 4%, P <.05) and 10 Hz (-33% +/- 5%, P <.05) in heart failure rats [4].
The glomerular filtration rate, urinary flow rate, and sodium excretion responses to renal sympathetic nerve stimulation were not affected by high-dose H 409/22 in either normal or heart failure rats [4].

Biological context of H 409-22

In the guinea pig, the Y2-receptor-preferring fragment NPY(3-36) and the selective Y1-receptor antagonist H 409/22 were used to confirm that the increase in blood pressure was mediated solely through the Y1-receptor and the vagal inhibition solely through the Y2-receptor [5].
In anesthetized normal rats, the NPY Y(1) receptor antagonist, H 409/22, at two doses, had no effect on heart rate, arterial pressure, or renal hemodynamic and excretory function [4].

Gene context of H 409-22

In vivo characterization of the novel neuropeptide Y Y1 receptor antagonist H 409/22 [6].

References

Receptor subtypes Y1 and Y5 mediate neuropeptide Y induced feeding in the guinea-pig. Lecklin, A., Lundell, I., Paananen, L., Wikberg, J.E., Männistö, P.T., Larhammar, D. Br. J. Pharmacol. (2002) [Pubmed]
Neuropeptide Y Y(5) receptor antagonist CGP71683A: the effects on food intake and anxiety-related behavior in the rat. Kask, A., Vasar, E., Heidmets, L.T., Allikmets, L., Wikberg, J.E. Eur. J. Pharmacol. (2001) [Pubmed]
Neuropeptide Y Y1 receptor mediated mesenteric vasoconstriction in the pig in vivo. Malmström, R.E. Regul. Pept. (2000) [Pubmed]
Role of neuropeptide Y in renal sympathetic vasoconstriction: studies in normal and congestive heart failure rats. DiBona, G.F., Sawin, L.L. J. Lab. Clin. Med. (2001) [Pubmed]
Neuropeptide Y1- and Y2-receptor-mediated cardiovascular effects in the anesthetized guinea pig, rat, and rabbit. Abrahamsson, C. J. Cardiovasc. Pharmacol. (2000) [Pubmed]
In vivo characterization of the novel neuropeptide Y Y1 receptor antagonist H 409/22. Malmström, R.E., Alexandersson, A., Balmér, K.C., Weilitz, J. J. Cardiovasc. Pharmacol. (2000) [Pubmed]

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